Chemotherapy 2 Flashcards
Temozolomide MOA
Bioactivated into diazomethane which methylates DNA
Temozolomide Thera use
Brain (astrocytoma), Melanoma
Temozolomide side effects
BMS (thrombocytopenia, neutropenia), HA, Fatigue
Temozolomide MOR
Alkyl guanine transferase
Cisplatin MOA
Forms DNA adducts which inhibit DNA replication & transcription & lead to breaks & miscoding, N7 guanine
Cisplatin Thera use
Testicular, Ovarian, Cervix, Bladder, N/SCLC
Cisplatin side effects
BMS, Peripheral neuropathy, Ototoxicity, Hypersentivity rxn (Anaphylaxis) Nephrotoxicity (decrease w/ NS hydration, diuresis, Amifostine: cytoprotective)
Cisplatin MOR
Loss of mismatch repair (MMR) ->no apoptosis
Methotrexate MOA
Inhibition of Dihydrofolate reductase: decrease DNA, RNA synthesis, S phase specific
Methotrexate therapeutic use
ALL, CNS leukemia (IT), GTN, Breast, NHL
Methotrexate side effects
Myelosuppression, pneumonitis, mucositis, hepatoxicity, nephrotoxicity, teratogenesis, meningismus (IT)
Methotrexate MOR
DHFR gene amplification
Pyrimidine analogs MOA
S-phase specific
5-FU → 5-F-deoxyuridine monophosphate, Inhibitor of thymidylate synthase -> decreases DNA synthesis
Pyrimidine analogs therapeutic use
5-FU: Colorectal, breast, gastric, pancreatic, esophageal
Pyrimidine analogs side effects
5-FU, Capecitabine: N/V/D, Alopecia, Myelosuppression, Hand & Foot syndrome
Purine analogs MOA
S-phase specific
6-MP → 6-thioguanine nucleotides, Incorporated in DNA & RNA, Cytotoxicty by decreased RNA & DNA synthesis
Purine analogs Therapeutic Uses:
6-MP: ALL
Purine analogs side effects
6-MP : Myelosuppression, N/V/D, Hepatotoxic
Vincristine MOA
Block cells in mitosis, M-phase specific, bind specifically to tubulin & block its ability to polymerize into microtubules
Vincristine Therapeutic Uses
HD, NHL, Brain, ALL
Vincristine Side Effects
Fatal (IT, seizures, coma), Alopecia, Myelosuppression, Neurotoxicity (paresthesia, PN), Constipation (ileus), SIADH
Vincristine MOR
MDR, MRP, Tubulin mutations
Paclitaxel MOA
Bind to microtubules & antagonize the disassembly, causes arrest in mitosis, M phase specific
Paclitaxel Thera uses
Ovarian, N/SCLC, Breast, H/N, KS
Paclitaxel side effects
Myelosuppression, Peripheral neuropathy, Mucositis (ulcers), Hypersensitivity (50:50 Etoh:Castor oil)
Paclitaxel MOR
MDR, Tubulin mutations